cilastatin

Cilastatin is a small molecule inhibitor of renal dehydropeptidase-I, an enzyme located in the brush border of the renal tubule. Its primary use is to prevent the degradation of certain beta-lactam antibiotics, most notably imipenem, by inhibiting this enzyme. Cilastatin itself does not possess antibiotic activity but is co-administered with imipenem to prolong and enhance its antibacterial effect by preventing its breakdown in the kidneys. The first combination product containing both drugs was approved under the trade name Primaxin and marketed by Merck & Co., with a newer triple-drug product (Recarbrio) also available[1][5][6]. Cilastatin may also inhibit some bacterial metallo-beta-lactamases due to structural similarities with its main target[5].

Brand names

PrimaxinRecarbrio

Other names

DPEP-1 inhibitorDPEP1 inhibitorDPEP 1 inhibitorDHP-I inhibitordehydropeptidase-I inhibitor